Chemoselective methionine 18F-fluorination on unprotected peptides for positron-emission tomography imaging
| Project/Area Number |
19K17156
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| Research Category |
Grant-in-Aid for Early-Career Scientists
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| Allocation Type | Multi-year Fund |
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| Review Section |
Basic Section 52040:Radiological sciences-related
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| Research Institution | National Institutes for Quantum Science and Technology |
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Principal Investigator |
Hu Kuan 国立研究開発法人量子科学技術研究開発機構, 量子医科学研究所 先進核医学基盤研究部, 研究員 (00827678)
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| Project Period (FY) |
2019-04-01 – 2022-03-31
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| Project Status |
Discontinued (Fiscal Year 2021)
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| Budget Amount *help |
¥4,160,000 (Direct Cost: ¥3,200,000、Indirect Cost: ¥960,000)
Fiscal Year 2021: ¥910,000 (Direct Cost: ¥700,000、Indirect Cost: ¥210,000)
Fiscal Year 2020: ¥1,690,000 (Direct Cost: ¥1,300,000、Indirect Cost: ¥390,000)
Fiscal Year 2019: ¥1,560,000 (Direct Cost: ¥1,200,000、Indirect Cost: ¥360,000)
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| Keywords | peptide / fluorine 18 / radiolabeling / PET / cancer / diagnosis / methionine / 18F-fluorination / chemoselective / ReACT / oxaziridine / radiotracer / Peptide / PET tracer / ozaxiridine / 18F labeling / 18F bioconjugatoin / Methionine / PET imaging |
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| Outline of Research at the Start |
A strategy for chemoselective radio-methionine bioconjugation through a redox-activated chemical tagging (ReACT), using oxaziridine-based 18F-reagent to achieve highly selective, rapid, and robust methionine labeling under biocompatible reaction conditions.
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| Outline of Final Research Achievements |
PET imaging is a highly clinically relevant technique for disease diagnosis. A series of PET radiotracers have been approved for clinical use. As one class of PET tracers, peptide-based radiotracers have many advantages due to their favorable pharmacokinetics and biodistribution profiles. The development of peptide-based PET tracers is emerging as one of the most vital task for nuclear medicine, while the direct labeling of unprotected peptides without prothestic group remains a challenge. 18F is an positron emission radionuclide with a decay hald-life of 109.8 min, showing a good matchness with the biological half-life of peptides. In this context, the radiolabeling of peptide with 18F is attracting more and more attention from both industry and acedamia. In this project, we developed a non-prothestic, bioconjugated method for direct 18F labeling of unprotected peptides with methionine residues.The method is generally applicable for radiolabeling any Met-containing peptides.
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| Academic Significance and Societal Importance of the Research Achievements |
This resarch results may help develop imaging agents that can be used for disease diagnosis in hospticals. Our research provide a feasible method to synthesize imaging agents via an more financially econimic way, thus save cost for patients.Moreover, it can reduce radiation to the human body.
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Report
(3 results)
Research Products
(34 results)
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[Presentation] Positron Emission Tomography Imaging of Vascular Endothelial Growth Factor Receptor Expression with a new 64Cu labeled peptide2020
Author(s)
Hu, Kuan Shang, Jingjie Xie, Lin Hanyu, Masayuki Zhang, Yiding Yang, Zhimin Yang, Zhimin Xu, Hao Wang, Lu Zhang, Ming-Rong
Organizer
SNMMI 2020 Annual Meeting
Related Report
Int'l Joint Research
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[Presentation] Development of novel 18F-labeled PET tracers for imaging TSPO with insensitivity to rs6971 polymorphism2020
Author(s)
Lingling Zhang , Masayuki Fujinaga , Bin Ji , Hu Kuan , Weijian Ye , Lin Xie , Yiding Zhang , Lu Hou , Hao Xu , Ming-Rong Zhang , Wang Lu
Organizer
SNMMI 2020 Annual Meeting
Related Report
Int'l Joint Research
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[Presentation] 癌蛋白質mGluR1に基づくがん種横断的な211At-AITM標的アイソトープ治療法の開発2020
Author(s)
謝 琳 , 張 露露 , 破入 正行 , 藤永 雅之 , 張 一鼎 , 峯岸 克行 , Hu Kuan , 李 惠子 , 長谷川 純崇 , 永津 弘太郎 , 張 明栄
Organizer
第60回日本核医学会学術総会
Related Report
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